Home Hippo MAP4K inhibitor DMX-5084

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DMX-5084 MAP4K inhibitor

Cat.No.S0268

DMX-5804 is a potent, orally active and selective inhibitor of Mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4) with IC50 of 3 nM for human MAP4K4. DMX-5804 is more potent on human MAP4K4 with pIC50 of 8.55 than MINK1/MAP4K6 and TNIK/MAP4K7 with pIC50 of 8.18 and 7.96, respectively.
DMX-5084 MAP4K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 361.39

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S026801 DMSO]72 mg/mL]false]Ethanol]1.5 mg/mL]false]Water]Insoluble]false Purity: 99.69%
99.69

Chemical Information, Storage & Stability

Molecular Weight 361.39 Formula

C21H19N3O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 2306178-56-1 -- Storage of Stock Solutions

Synonyms N/A Smiles COCCOC1=CC=C(C=C1)C2=CN(C3=C2C(=O)NC=N3)C4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 72 mg/mL ( (199.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1.5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
human MAP4K4 [1]
(Cell-free assay)
8.55(pIC50)
human MAP4K4 [1]
(Cell-free assay)
3 nM
MINK1/MAP4K6 [1]
(Cell-free assay)
8.18(pIC50)
TNIK/MAP4K7 [1]
(Cell-free assay)
7.96(pIC50)
References

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